The laxative effect of emodin is attributable to increased aquaporin 3 expression in the colon of mice and HT-29 cells

Fitoterapia. 2014 Jul:96:25-32. doi: 10.1016/j.fitote.2014.04.002. Epub 2014 Apr 13.

Abstract

Emodin (1,3,8-trihydroxy-6-methylanthraquinone) is a stimulant laxative and used to treat constipation. Aquaporin 3 (AQP3) plays an important role in regulating water transfer in the colon. In the study, we investigated whether the laxative effect of emodin is associated with the regulation of AQP3 in the colon. Our results showed that treatment with emodin increased the fecal water content in the colon of mice and evaluation index of defecation in a dose-dependent manner. More interestingly, emodin significantly increased the AQP3 protein and mRNA expression both in the colon of mice and in human intestinal epithelial cells (HT-29). Mechanistically, emodin obviously up-regulated the cyclic adenosine monophosphate (cAMP)-dependent protein kinase A catalytic subunits α (PKA C-α) and phosphorylated cAMP response element-binding protein (p-CREB Ser133) expression in HT-29 cells. These results suggest that the laxative effect of emodin is associated with the increased expression of AQP3 by up-regulating PKA/p-CREB signal pathway.

Keywords: Aquaporin 3; Colon; Emodin; Laxative.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aquaporin 3 / genetics
  • Aquaporin 3 / metabolism*
  • Cell Survival / drug effects
  • Colon / drug effects
  • Diarrhea / chemically induced
  • Dose-Response Relationship, Drug
  • Emodin / chemistry
  • Emodin / isolation & purification
  • Emodin / pharmacology*
  • Epithelial Cells / drug effects
  • Feces / chemistry
  • Gene Expression Regulation / drug effects*
  • HT29 Cells
  • Humans
  • Laxatives / chemistry
  • Laxatives / isolation & purification
  • Laxatives / pharmacology*
  • Male
  • Mice
  • Mice, Inbred ICR
  • Molecular Structure
  • Signal Transduction / drug effects*
  • Up-Regulation / drug effects
  • Water / metabolism

Substances

  • AQP3 protein, human
  • Aqp3 protein, mouse
  • Laxatives
  • Water
  • Aquaporin 3
  • Emodin